-
morphine
- opioid agonist
- renal excretion (phase II - glucuronidation)
- metabolites: M6G (5-10%, 10x more potent), M3G (70-80%, no analgesia)
-
hydromorphone
- opioid agonist
- renal excretion (phase II - glucuronidation)
- metabolites: H6G, H3G
-
fentanyl
- opioid agonist
- hepatic metabolism (CYP3A4)
-
oxycodone
- opioid agonist
- hepatic metabolism (CYP2D6, CYP3A4)
- active metabolites
-
naloxone
- competitive antagonist at MOR, DOR, KOR with high affinity for MOR but no efficacy
- no oral absorption, but mixed with oral opioid as abuse deterrent, blocks MOR in gut
- IV or IM blocks peripheral and central MOR
- onset within seconds, very short half-life
-
naltrexone
- competitive antagonist at MOR, DOR, KOR with high affinity for MOR but no efficacy
- oral, longer duration of action
- new long-acting IM depot product for opioid or alcohol addiction
-
buprenorphine
- high affinity, partial agonist for MOR
- initial opioid response, but plateaus
- ceiling effect on analgesia and resp depression
- long dissociation - used for opioid addiction (w or w/o naloxone)
- may precipitate withdraw if added to full agonist
-
Tramadol
- weak opioid agonist (MOR)
- serotonin and NE reuptake inhibitor
-
nalbuphine
- agonist-antagonist
- high MOR affinity, poor MOR efficacy to the point of possible antagonist activity
- KOR agonist
- complex usage
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